公开(公告)号：US20080081817A1

公开(公告)日：2008-04-03

申请号：US11632725

申请日：2005-07-22

申请人： Iwao Takamuro ,  Saburo Kawanami ,  Yasunori Tsuboi ,  Toshiyuki Himiyama ,  Yuko Hasegawa ,  Hideki Mochida ,  Kouji Nogi

发明人： Iwao Takamuro ,  Saburo Kawanami ,  Yasunori Tsuboi ,  Toshiyuki Himiyama ,  Yuko Hasegawa ,  Hideki Mochida ,  Kouji Nogi

IPC分类号： A61K31/497 ,  A61K31/519 ,  A61P43/00 ,  C07D401/00 ,  C07D487/00

CPC分类号： C07D471/04 ,  C07D487/04

摘要： A novel nitrogenous fused bicyclic compound represented by the following general formula [1] or a pharmacologically acceptable salt of the compound. They have excellent SK channel blocking activity and are useful as a medicine. [I] (In the formula, R0 represents hydrogen, halogeno, etc.; R1 represents a group represented by the formula (a) or (b); A represents a group represented by the formula (X) or (Y); D1, D2 and D3 each represents N or CH; R2 represents halogeno or optionally halogenated lower alkyl, etc.; R3 represents hydrogen or lower alkyl; and Q represents lower alkylene.)

摘要翻译： 由以下通式[1]表示的新型含氮稠合双环化合物或该化合物的药理学上可接受的盐。 它们具有优异的SK通道阻断活性，可用作药物。 [I]（式中，R 0表示氢，卤素等; R 1表示由式（a）或（b）表示的基团; A 表示由式（X）或（Y）表示的基团; D 1，D 2和D 3各自表示N或CH; R 2表示卤代或任选卤代的低级烷基等; R 3表示氢或低级烷基; Q表示低级亚烷基。）

公开(公告)号：US20110166135A1

公开(公告)日：2011-07-07

申请号：US13062841

申请日：2009-09-09

申请人： Hiroshi Morimoto ,  Toshiaki Sakamoto ,  Toshiyuki Himiyama ,  Eiji Kawanishi ,  Takehiko Matsumura

发明人： Hiroshi Morimoto ,  Toshiaki Sakamoto ,  Toshiyuki Himiyama ,  Eiji Kawanishi ,  Takehiko Matsumura

IPC分类号： A61K31/5377 ,  C07D401/14 ,  C07D487/04 ,  C07D413/14 ,  A61K31/517 ,  A61K31/506 ,  A61K31/497 ,  A61K31/519 ,  A61P25/18 ,  A61P25/24 ,  A61P25/22 ,  A61P25/16 ,  A61P25/28

CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12

摘要： The present invention provides aromatic nitrogen-containing 6-membered ring compounds having excellent PDE10 inhibitory activity. The present invention relates to an aromatic nitrogen-containing 6-membered ring compound represented by the following formula [I0] or a pharmaceutically acceptable salt thereof, a method for preparing the same, and use of said compounds for PDE10 inhibitors, and a pharmaceutical composition comprising said compounds as an active ingredient: Formula [I0] wherein: X1, X2 and X3 each independently are N or CH, and at least two of X1, X2 and X3 are N; A is *—CH═CH—, *—C(Alk)=CH—, *—CH2—CH2— or *—O—CH2— (* is a bond with R1); Alk is a lower alkyl group; Ring B is an optionally substituted nitrogen-containing aliphatic heterocyclic group; R1 is an optionally substituted nitrogen-containing heterocyclic group, a nitrogen-containing heterocyclic moiety of which is a moiety selected from the group consisting of quinoxalinyl, quinolyl, isoquinolyl, quinazolinyl, pyrazinyl, pyrimidinyl and a moiety thereof fused with a 5 to 6-membered aliphatic ring thereto; Y0 is a group selected from the group consisting of the following (1) to (5): (1) an optionally substituted phenyl or an optionally substituted aromatic monocyclic 5 to 6-membered heterocyclic group; (2) an optionally substituted aminocarbonyl; (3) an optionally substituted amino lower alkyl; (4) —O—R2 wherein R2 is hydrogen, an optionally substituted lower alkyl, lower cycloalkyl, aliphatic monocyclic 5 to 6-membered heterocyclic group, or Formula [AA]; (5) mono- or di-substituted amino; provided that, when Y0 is mono- or di-substituted amino, the nitrogen-containing heterocyclic moiety of R1 is not quinoxalinyl or quinolyl.

摘要翻译： 本发明提供具有优异的PDE10抑制活性的芳香族含氮6元环化合物。 本发明涉及由下式[I0]表示的含芳族含氮的6元环化合物或其药学上可接受的盐，其制备方法以及所述化合物用于PDE10抑制剂的用途和药物组合物 包括所述化合物作为活性成分：式[I0]其中：X1，X2和X3各自独立地为N或CH，X1，X2和X3中的至少两个为N; A是* -CH = CH-，* -C（Alk）= CH-，* -CH2-CH2-或* -O-CH2-（*是与R1的键）; Alk是低级烷基; 环B是任选取代的含氮脂族杂环基; R1是任选取代的含氮杂环基团，其含氮杂环部分是选自喹喔啉基，喹啉基，异喹啉基，喹唑啉基，吡嗪基，嘧啶基及其部分与5至6位稠合的部分， 元环脂族环; Y0是选自下列（1）至（5）的基团：（1）任选取代的苯基或任选取代的芳族单环5至6元杂环基; （2）任选取代的氨基羰基; （3）任选取代的氨基低级烷基; （4）-O-R2，其中R2是氢，任选取代的低级烷基，低级环烷基，脂族单环5至6元杂环基或式[AA]; （5）单取代或二取代氨基; 条件是当Y 0是单取代或二取代的氨基时，R 1的含氮杂环部分不是喹喔啉基或喹啉基。